Patent classifications
C07D497/08
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-8 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
Heterocyclic compounds useful as pim kinase inhibitors
The present application is concerned with heterocyclic compounds that inhibit the activity of Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancers and other diseases.
PYRIDINYL DERIVATIVES AS SODIUM CHANNEL ACTIVATORS
The present disclosure is directed to compounds of formula (I):
##STR00001##
wherein X, Y, Z, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, and L are as described herein, as stereoisomers, enantiomers, or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates, or prodrugs thereof, and pharmaceutical compositions comprising the compounds of formula (I), as described herein, which are useful as voltage-gated sodium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.
PYRIDINYL DERIVATIVES AS SODIUM CHANNEL ACTIVATORS
The present disclosure is directed to compounds of formula (I):
##STR00001##
wherein X, Y, Z, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, and L are as described herein, as stereoisomers, enantiomers, or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates, or prodrugs thereof, and pharmaceutical compositions comprising the compounds of formula (I), as described herein, which are useful as voltage-gated sodium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.
Compound having perfluoroalkyl terminal group and CF2O bonding group, liquid crystal composition and liquid crystal display device
The subject is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat or light, a high clearing point (or a high maximum temperature), a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectic anisotropy, a suitable elastic constant and an excellent compatibility with any other liquid crystal compound, a liquid crystal composition including this compound and a liquid crystal display device including this composition. The compound is represented by the following formula (1a): ##STR00001##
wherein R.sup.1 is alkyl having 1 to 15 carbons or the like; ring A.sup.1, ring A.sup.2, ring A.sup.3 and ring A.sup.4 are independently 1,4-phenylene, naphthalene-2,6-diyl or the like; Z.sup.1 and Z.sup.2 are independently a single bond or the like; o and p are independently 0, 1 or 2; and n is an integer from 2 to 10.
Compound having perfluoroalkyl terminal group and CF2O bonding group, liquid crystal composition and liquid crystal display device
The subject is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat or light, a high clearing point (or a high maximum temperature), a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectic anisotropy, a suitable elastic constant and an excellent compatibility with any other liquid crystal compound, a liquid crystal composition including this compound and a liquid crystal display device including this composition. The compound is represented by the following formula (1a): ##STR00001##
wherein R.sup.1 is alkyl having 1 to 15 carbons or the like; ring A.sup.1, ring A.sup.2, ring A.sup.3 and ring A.sup.4 are independently 1,4-phenylene, naphthalene-2,6-diyl or the like; Z.sup.1 and Z.sup.2 are independently a single bond or the like; o and p are independently 0, 1 or 2; and n is an integer from 2 to 10.